S7023 |
Z-VAD-FMK
|
Z-VAD-FMK (Z-VAD(OMe)-FMK) is a cell-permeable, irreversible pan-caspase inhibitor, blocks all features of apoptosis in THP.1 and Jurkat T-cells. |
-
Nature, 2024, 626(7998):411-418.
-
Nature, 2024, 626(7998):411-418.
-
Cell, 2024, 187(15):4061-4077.e17
|
|
S1029 |
Lenalidomide
|
Lenalidomide is a TNF-α secretion inhibitor with IC50 of 13 nM in PBMCs. Lenalidomide (CC-5013) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide promotes cleaved caspase-3 expression and inhibit VEGF expression and induces apoptosis. |
-
Nat Commun, 2024, 15(1):9559
-
Nat Commun, 2024, 15(1):7388
-
Clin Immunol, 2024, 260:109915
|
|
S2768 |
Dinaciclib
|
Dinaciclib is a novel and potent CDK inhibitor for CDK2, CDK5, CDK1 and CDK9 with IC50 of 1 nM, 1 nM, 3 nM and 4 nM in cell-free assays, respectively. It also blocks thymidine (dThd) DNA incorporation. Dinaciclib induces apoptosis through the activation of caspases 8 and 9. Phase 3. |
-
Cell Death Dis, 2024, 15(4):285
-
Cell Death Dis, 2024, 15(5):345
-
Cell Death Dis, 2024, 15(4):285
|
|
S2228 |
Belnacasan (VX-765)
|
Belnacasan (VX-765) is a potent and selective inhibitor of caspase-1 with Ki of 0.8 nM in a cell-free assay. Phase 2. |
-
Journal of Environmental Sciences, 2025, Volume 148
-
Mol Cancer, 2024, 23(1):240
-
Nat Commun, 2024, 15(1):8266
|
|
S7312 |
Z-DEVD-FMK
|
Z-DEVD-FMK (Caspase-3 Inhibitor) is a specific, irreversible Caspase-3 inhibitor, and also shows potent inhibition on caspase-6, caspase-7, caspase-8, and caspase-10. |
-
Cell Rep Med, 2024, 5(3):101476
-
J Immunother Cancer, 2024, 12(10)e009032
-
Cancer Lett, 2024, 588:216797
|
|
S7311 |
Q-VD-Oph
|
Q-VD-Oph (Quinoline-Val-Asp-Difluorophenoxymethylketone) is a potent pan-caspase inhibitor with IC50 ranged from 25 to 400 nM for caspases 1,3,8, and 9. Q-VD-OPh can inhibits HIV infection. |
-
Nat Commun, 2024, 15(1):830
-
Cell Death Dis, 2024, 15(5):363
-
Cell Death Discov, 2024, 10(1):125
|
|
S7314 |
Z-IETD-FMK
|
Z-IETD-FMK (Caspase-8 Inhibitor, Z-IE(OMe)TD(OMe)-FMK) is a specific Caspase-8 inhibitor. Z-IETD-FMK is also an inhibitor of granzyme B. |
-
Nat Commun, 2024, 15(1):1282
-
J Immunother Cancer, 2024, 12(10)e009032
-
Mol Metab, 2024, 87:101988
|
|
S7775 |
Emricasan (IDN-6556)
|
Emricasan (IDN-6556, PF 03491390, PF-03491390) is a potent irreversible pan-caspase inhibitor. Emricasan is an inhibitor of Zika virus infection. |
-
Immunity, 2024, S1074-7613(24)00221-8
-
Acta Neuropathol, 2024, 147(1):56
-
Cell Death Differ, 2024, 31(7):938-953
|
|
S7901 |
Ac-DEVD-CHO
|
Ac-DEVD-CHO (Caspase-3 Inhibitor I, N-Ac-Asp-Glu-Val-Asp-CHO) is a potent aldehyde inhibitor of Group II caspases with Ki values of 0.2 nM and 0.3 nM for for caspase-3 and caspase-7, respectively. Weak inhibition for caspase-2. |
-
Environ Pollut, 2024, 345:123467
-
Int J Mol Sci, 2024, 25(1)627
-
Cell, 2023, 186(14):3033-3048.e20
|
|
S7313 |
Z-LEHD-FMK TFA
|
Z-LEHD-FMK TFA (Caspase-9 Inhibitor) is a cell-permeable, competitive and irreversible inhibitor of enzyme caspase-9, which helps in cell survival. |
-
Front Immunol, 2024, 15:1384606
-
Ecotoxicol Environ Saf, 2024, 284:116944
-
PLoS Pathog, 2024, 20(4):e1012146
|
|
S8102 |
Z-VAD(OH)-FMK (Caspase Inhibitor VI)
|
Z-VAD(OH)-FMK (Caspase Inhibitor VI) is an irreversible pan-caspase inhibitor. |
-
Cell, 2024, 187(15):4043-4060.e30
-
Nat Commun, 2024, 15(1):9464
-
J Ethnopharmacol, 2024, 328:118057
|
|
S2891 |
GW441756
|
GW441756 is a potent, selective inhibitor of TrkA with IC50 of 2 nM, with very little activity to c-Raf1 and CDK2. GW441756 produces a relevant increase of caspase-3 that leads to apoptosis. |
-
Cells, 2023, 12(3)373
-
Cells, 2023, 12(3):373
-
J Cell Mol Med, 2023, 10.1111/jcmm.17906
|
|
S2738 |
PAC-1
|
PAC-1 is a potent procaspase-3 activator with EC50 of 0.22 μM and the first small molecule known to directly activate procaspase-3 to caspase-3. |
-
Nat Commun, 2023, 14(1):5773
-
Nat Commun, 2023, 14(1):5773
-
Microb Cell, 2023, 10(8):157-169
|
|
S8507 |
Z-YVAD-FMK
|
Z-YVAD-FMK is a cell-permeable and irreversible caspase-1 specific inhibitor with anti-inflammatory and anti-tumor activities. |
-
Transl Psychiatry, 2024, 14(1):166
-
EMBO J, 2023, e113118.
-
J Nanobiotechnology, 2023, 21(1):426
|
|
S2927 |
Apoptosis Activator 2
|
Apoptosis Activator 2 strongly induces caspase-3 activation, PARP cleavage, and DNA fragmentation which leads to the destruction of cells (Apaf-1 dependent) with IC50 of ~4 μM, inactive to HMEC, PREC, or MCF-10A cells. |
-
BMC Mol Cell Biol, 2023, 24(1):14
-
BMC Mol Cell Biol, 2023, 24(1):14
-
Antioxidants (Basel), 2021, 10(2)184
|
|
S2417 |
20-Hydroxyecdysone
|
20-Hydroxyecdysone (Ecdysterone, 20E, B-ecdysone, Commisterone, Crustecdysone) is a naturally occurring ecdysteroid hormone which controls the ecdysis (moulting) and metamorphosis of arthropods.20-Hydroxyecdysone (Ecdysterone, 20E) inhibits caspase activity and induces autophagy via the 20E nuclear receptor complex, EcR-USP. |
-
bioRxiv, 2024, 10.1101/2024.01.04.574133
-
Appl Sci, 2023, 13(2), 860
-
Biomed Environ Sci, 2022, 35(6):504-517
|
|
S2448 |
Gambogic Acid
|
Gambogic Acid (Guttatic Acid, Guttic Acid, Beta-Guttiferrin) activates caspases with EC50 of 0.78-1.64 μM and competitively inhibits Bcl-XL, Bcl-2, Bcl-W, Bcl-B, Bfl-1 and Mcl-1 with IC50 of 1.47, 1.21, 2.02, 0.66, 1.06 and 0.79 μM, respectively. |
-
Cells, 2023, 12(18)2247
-
Cells, 2023, 10.3390/cells12182247
-
Cancers (Basel), 2022, 14(22)5505
|
|
S9042 |
Wedelolactone
|
Wedelolactone, a medicinal plant-derived natural compound, is an inhibitor of IKK that is critical for activation of NF-κB by mediating phosphorylation and degradation of IκBα. Wedelolactone is also an inhibitor of caspase-11. |
-
Int J Ophthalmol, 2024, 17(4):616-624
-
PeerJ, 2022, 10:e13766
-
Exp Eye Res, 2021, 211:108750
|
|
S3275 |
Senkyunolide I
|
Senkyunolide I (SEI, SENI) is an orally active compound isolated from Ligusticum chuanxiong with analgesic, anti-migraine, neuroprotective, anti-oxidation and anti-apoptosis activities. Senkyunolide I (SEI, SENI) up-regulates the phosphorylation of Erk1/2 and induces Nrf2 nuclear translocation with enhanced HO-1 and NQO1 expressions. Senkyunolide I (SEI, SENI) promotes the ratio of Bcl-2/Bax and inhibits the expressions of cleaved caspase 3 and caspase 9. |
-
World J Emerg Med, 2024, 15(3):206-213
-
SSRN , 2024, 10.2139/ssrn.4696834
-
Cancer Biol Med, 2022, 19(11)j.issn.2095-3941.2022.0451
|
|
S5967 |
Berberine chloride hydrate
|
Berberine (Natural Yellow 18) chloride hydrate is a quaternary ammonium salt from the group of isoquinoline alkaloids. Berberine activates caspase 3 and caspase 8, cleavage of poly ADP-ribose polymerase (PARP) and the release of cytochrome c. Berberine chloride decreases the expression of c-IAP1, Bcl-2 and Bcl-XL. Berberine chloride induces apoptosis with sustained phosphorylation of JNK and p38 MAPK, as well as generation of the ROS. Berberine chloride is a dual topoisomerase I and II inhibitor. Berberine chloride is also a potential autophagy modulator. |
-
Front Biosci (Landmark Ed), 2022, 27(8):242
-
Front Pharmacol, 2021, 12:632201
|
|
S3865 |
Taurochenodeoxycholic acid
|
Taurochenodeoxycholic acid (Taurochenodeoxycholate, TCDCA, Chenodeoxycholyltaurine), a bile acid formed in the liver of most species, is used as a cholagogue and choleretic. |
-
Nat Commun, 2021, 12(1):6479
-
Microbiome, 2019, 7(1):145
|
|
S7326 |
Tasisulam
|
Tasisulam (LY573636) is an antitumor agent and an apoptosis inducer via the intrinsic pathway. Phase 3. |
-
Skin Pharmacol Physiol, 2016, 29(6):281-290
|
|
S3238 |
Resibufogenin
|
Resibufogenin (Bufogenin, Recibufogenin), a component of huachansu with anticancer effect, triggers necroptosis through upregulating receptor-interacting protein kinase 3 (RIP3) and phosphorylating mixed lineage kinase domain-like protein at Ser358. Resibufogenin exerts cytotoxic effect by inducing reactive oxygen species (ROS) accumulation. Resibufogenin induces apoptosis and caspase-3 and caspase-8 activity. Resibufogenin increases Bax/Bcl-2 expression, and suppresses cyclin D1, cyclin E, PI3K, p-AKT, p-GSK3β and β-catenin protein expression. |
-
Research Square, 2024, 10.21203/rs.3.rs-3790060/v1
-
Phytomedicine, 2022, 102:154182
|
|
S0563 |
10-Deacetyl-7-xylosyl paclitaxel
|
10-Deacetyl-7-xylosyl paclitaxel (10-Deacetyl-7-xylosyltaxol, 7-xylosyl-10-deacetylpaclitaxel), a derivative of paclitaxel and naturally occurring xyloside isolated from Taxus chinensis, causes significant mitotic arrest in PC-3 cells followed by up-regulating expression of pro-apoptotic Bax and Bad protein, as well as down-regulating expression of anti-apoptotic Bcl-2 and Bcl-XL , which leads to a disturbance of the mitochondrial membrane permeability and to the activation of caspase-9. |
-
Cell Death Dis, 2022, 13-9:799
|
|
S8487 |
AP20187
|
AP20187 (B/B Homodimerizer) is a chemical inducer of dimerization that activates FKBP-Casp8. |
-
Front Immunol, 2022, 13:1110322
|
|
S9817 |
Ac-FLTD-CMK
|
Ac-FLTD-CMK is a specific inhibitor for inflammatory caspases. Ac-FLTD-CMK inhibits gasdermin D (GSDMD) cleavage by caspases-1, -4, -5, and -11 in vitro. Ac-FLTD-CMK is effective against caspases-1, caspases-4 and caspases-5 with IC50 of 46.7 nM, 1.49 μM and 329 nM, respectively. |
-
Cell Death Discov, 2024, 10(1):416
-
Biomolecules, 2022, 12(11)1660
|
|
S9634 |
Phenoxodiol (Haginin E)
|
Phenoxodiol (Haginin E, Idronoxil, Dehydroequol, NV 06, PXD) is an isoflavone analog with antineoplastic activity that activates the caspase system, inhibits XIAP (X-linked inhibitor of apoptosis), and disrupts FLICE inhibitory protein (FLIP) expression, resulting in tumor cell apoptosis. Phenoxodiol also inhibits DNA topoisomerase II. |
-
Anticancer Res, 2018, 38(10):5709-5716
|
|
E3037 |
Solanum lyratum Extract
|
Solanum lyratum Extract (300 μg/ml) increases Bax levels and decreases Bcl-2 levels, which cause the loss of mitochondrial membrane potential (Δæm) followed by cytochrome C release and caspase-9 and -3 activation, finally leading to apoptosis. Solanum lyratum Extract (300 μg/ml) also promotes p53 and p27, but decreases the levels of cyclin B1 thus causing S-phase arrest. |
|
|
S6899 |
Licochalcone D
|
Licochalcone D (Lico D, LCD, LD), a flavonoid isolated from a Chinese medicinal plant Glycyrrhiza inflata, has antioxidant, anti-inflammatory and anti-cancer properties. Licochalcone D inhibit phosphorylation of NF-κB p65 in LPS signaling pathway. Licochalcone D inhibits JAK2, EGFR and Met (c-Met) activities and induces ROS-dependent apoptosis. Licochalcone D also induces caspases activation and poly (ADP-ribose) polymerase (PARP) cleavage. |
|
|
S0913 |
4',5,7-Trimethoxyflavone
|
4',5,7-Trimethoxyflavone (5,7,4'-Trimethoxyflavone, TMF) is a flavonoid isolated from Kaempferia parviflora (KP) that induces apoptosis. 4',5,7-Trimethoxyflavone increases sub-G1 phase, DNA fragmentation, annexin-V/PI staining and Bax/Bcl-xL ratio, activates caspase-3 and degrades poly (ADP-ribose) polymerase (PARP) protein. |
|
|
S6501 |
NVP 231
|
NVP 231 is a novel CerK inhibitor that inhibits the catalytic activity of recombinant CerK in vitro with an IC50 of 12 nM. NVP 231 induces cell apoptosis by increasing DNA fragmentation and caspase-3 and caspase-9 cleavage. |
|
|
S3224 |
Cinobufagin
|
Cinobufagin (Cinobufagine), an active ingredient of Venenum Bufonis, inhibits tumor development. Cinobufagin increases ATM and Chk2 and decreases CDC25C, CDK1, and cyclin B. Cinobufagin inhibits PI3K, AKT and Bcl-2 while increases levels of cleaved caspase-9 and caspase-3. Thus, Cinobufagin induces cell cycle arrest at the G2/M phase and apoptosis. |
|
|
E3053 |
Mentha Arvensis Leaf Extract
|
Mentha Arvensis Leaf Extract is extracted from the leaf of Mentha Arvensis, which might be considered as a promising anticancer agent in breast cancer therapy in combination with synthesised GSNPs because they are less toxic and nonmutagenic and mediate caspase 9-dependent apoptosis. |
|
|
E3835 |
Cordyceps Militaris Extract
|
Cordyceps Militaris Extract is extracted from Cordyceps militaris, which induces apoptosis and pyroptosis via caspase-3 and can be used as an anticancer agent. |
|
|
S3267 |
Nicotiflorin (Kaempferol-3-O-rutinoside)
|
Nicotiflorin (Kaempferol-3-O-rutinoside), a flavonoid extracted from Carthamus tinctorius, alters the shape and structure of injured neurons, decreases the number of apoptotic cells, down-regulates expression of p-JAK2, p-STAT3, caspase-3, and Bax and decreases Bax immunoredactivity, and increases Bcl-2 protein expression and immunoreactivity. |
|
|
E2354 |
Valepotriate
|
Valepotriate, an unstable iridoid isolated from Valeriana jatamansi Jones, has anti-epileptic by significantly increasing the expression of GABAA, glutamic acid decarboxylase 65, and Bcl-2 and reduce the expression of caspase-3. |
|
|
S9276 |
Alisol B
|
Alisol B, a triterpene from Alismatis rhizoma, induces Bax up-regulation and nuclear translocation, the activation of initiator caspase-8 and caspase-9, and executor caspase-3, suggesting the involvement of both extrinsic and intrinsic apoptosis pathways. |
|
|
S2271 |
Berberine chloride
|
Berberine chloride is a quaternary ammonium salt from the group of isoquinoline alkaloids. Berberine activates caspase 3 and caspase 8, cleavage of poly ADP-ribose polymerase (PARP) and the release of cytochrome c. Berberine chloride decreases the expression of c-IAP1, Bcl-2 and Bcl-XL. Berberine chloride induces apoptosis with sustained phosphorylation of JNK and p38 MAPK, as well as generation of the ROS. Berberine chloride is a dual topoisomerase I and II inhibitor. Berberine chloride is also a potential autophagy modulator. |
-
Adv Healthc Mater, 2023, e2300591.
-
Transl Oncol, 2023, 35:101712
-
J Biomol Struct Dyn, 2022, 1-11
|
|
S0354 |
Alsterpaullone
|
Alsterpaullone (Alp, 9-Nitropaullone, NSC 705701) is a potent inhibitor of CDK with IC50 of 35 nM, 15 nM, 200 nM and 40 nM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E and CDK5/p35, respectively. Alsterpaullone also acts as a potent inhibitor of glycogen synthase kinase-3 (GSK-3) with IC50 of both 4 nM for GSK-3α and GSK-3β. Alsterpaullone induces apoptosis by activation of caspase-9. Alsterpaullone has antitumor activity and possesses potential for the treatment of neurodegenerative and proliferative disorders. |
|
|
E3281 |
Eleutherine Plicata Extract
|
Eleutherine Plicata Extract is extracted from Eleutherine plicata, which is a promising medicinal plant, and its activity is associated with cytotoxicity by binding to caspase-8. |
|
|
E3638 |
Lysinotus pauciflorus Extract
|
Lysinotus Pauciflorus Extract is extracted from Lysinotus Pauciflorus, which induces apoptosis of hepatocellular carcinoma cells via caspase-3 mediated mitochondrial pathway. |
|
|
S6882 |
HI-TOPK-032
|
HI-TOPK-032 is a potent and specific inhibitor of TOPK. HI-TOPK-032 also reduces ERK-RSK phosphorylation, regulates of the abundance of p53, cleaved caspase-7, and cleaved PARP, and induces apoptosis in cancer cells. |
|
|
S4513 |
RGD peptide (GRGDNP)
|
RGD peptide (GRGDNP) is an inhibitor of binding of integrins to the extracellular matrixs. RGD peptide (GRGDNP) induces apoptosis presumably through direct activation of caspase-3. |
|
|
S9075 |
Mulberroside A
|
Mulberroside A, isolated from the ethanol extract of Morus alba roots, is widely employed as an active ingredient in cosmetic products due to its anti-tyrosinase and anti-oxidant activities. Mulberroside A decreases the expressions of TNF-α, IL-1β and IL-6 and inhibits the activation of NALP3, caspase-1 and NF-κB and the phosphorylation of ERK, JNK and p38. |
|
|
S3088 |
(±)-Methyl Jasmonate
|
(±)-Methyl Jasmonate (MeJA, Methyl jasmonate, Methyl 2-(3-oxo-2-(pent-2-en-1-yl)cyclopentyl)acetate), a phytohormone that acts as a vital cell regulator in plants, is a new candidate for the treatment of Inflammatory bowel diseases (IBDs), modulating the expression of the major classes of caspase-type protease families. |
|
|
S9097 |
Alisol B Acetate
|
Alisol B acetate, a triterpene from Alismatis rhizoma, induces Bax up-regulation and nuclear translocation, the activation of initiator caspase-8 and caspase-9, and executor caspase-3, suggesting the involvement of both extrinsic and intrinsic apoptosis pathways. |
|
|
S5550 |
Ethyl gallate
|
Ethyl gallat (Phyllemblin, gallic acid ethyl ester), which could be found naturally in a variety of plant sources, is a food additive with antimicrobial activity. Ethyl gallat activates the death receptor-dependent pathway of apoptosis by enhancing the expression of caspases-8, -9, and -3 and the Bcl-2 interacting domain (Bid). |
|
|
S5579 |
Chelidonic acid
|
Chelidonic acid (Jerva acid, Jervaic acid, γ-Pyrone-2,6-dicarboxylic acid) is a secondary metabolite found in several plants with therapeutic potential in allergic disorders in experimental animals. Chelidonic acid inhibits IL-6 production by blocking NF-κB and caspase-1 in HMC-1 cells. Chelidonic acid is also an inhibitor of glutamate decarboxylase with Ki of 1.2 μM. |
|
|
S6990 |
Phytohemagglutinin (PHA)
|
Phytohemagglutinin (PHA) is expressed in Pichia pastoris using native signal peptides, or the Saccharomyces alpha-factor preprosequence, to direct proteins into the secretory pathway. Phytohemagglutinin induces apoptosis in human HEp-2 carcinoma cells via increasing proapoptotic protein Bax and activating caspases-3. |
-
Molecules, 2023, 28(6)2426
|
|
S4353 |
Terfenadine
|
Terfenadine is an antihistamine, generally completely metabolizes to the active form fexofenadine in the liver by the enzyme cytochrome P450 CYP3A4 isoform. Terfenadine ((±)-Terfenadine) is a potent open-channel blocker of hERG with an IC50 of 204 nM. Terfenadine, an H1 histamine receptor antagonist, acts as a potent apoptosis inducer in melanoma cells through modulation of Ca2+ homeostasis. Terfenadine induces ROS-dependent apoptosis, simultaneously activates Caspase-4, -2, -9. |
|
|
S5584 |
Citronellol
|
Citronellol (Dihydrogeraniol, (±)-β-Citronellol), a constituent of rose and geranium oils, is used in perfumes and insect repellents. Citronellol can cause necrotic apoptosis of NCI-H1299 cells by up-regulating TNF-α, RIP1 / RIP3 activities, and down-regulating caspase-3 / caspase-8 activities. Citronellol also results in a biphasic increase in ROS production at 1 h and at 12 h in NCI-H1299 cells. |
|
|
S6846 |
Gly-Phe β-naphthylamide
|
Gly-Phe β-naphthylamide (Gly-Phe beta-naphthylamide) is a substrate of cathepsin C that accumulates within the lysosome. Gly-Phe-β-naphthylamide can inhibit the cathepsin-dependent activation of caspase-8. |
-
Anticancer Res, 2024, 44(9):3793-3798
|
|
S7023 |
Z-VAD-FMK
|
Z-VAD-FMK (Z-VAD(OMe)-FMK) is a cell-permeable, irreversible pan-caspase inhibitor, blocks all features of apoptosis in THP.1 and Jurkat T-cells. |
- Nature, 2024, 626(7998):411-418.
- Nature, 2024, 626(7998):411-418.
- Cell, 2024, 187(15):4061-4077.e17
|
|
S2228 |
Belnacasan (VX-765)
|
Belnacasan (VX-765) is a potent and selective inhibitor of caspase-1 with Ki of 0.8 nM in a cell-free assay. Phase 2. |
- Journal of Environmental Sciences, 2025, Volume 148
- Mol Cancer, 2024, 23(1):240
- Nat Commun, 2024, 15(1):8266
|
|
S7312 |
Z-DEVD-FMK
|
Z-DEVD-FMK (Caspase-3 Inhibitor) is a specific, irreversible Caspase-3 inhibitor, and also shows potent inhibition on caspase-6, caspase-7, caspase-8, and caspase-10. |
- Cell Rep Med, 2024, 5(3):101476
- J Immunother Cancer, 2024, 12(10)e009032
- Cancer Lett, 2024, 588:216797
|
|
S7311 |
Q-VD-Oph
|
Q-VD-Oph (Quinoline-Val-Asp-Difluorophenoxymethylketone) is a potent pan-caspase inhibitor with IC50 ranged from 25 to 400 nM for caspases 1,3,8, and 9. Q-VD-OPh can inhibits HIV infection. |
- Nat Commun, 2024, 15(1):830
- Cell Death Dis, 2024, 15(5):363
- Cell Death Discov, 2024, 10(1):125
|
|
S7314 |
Z-IETD-FMK
|
Z-IETD-FMK (Caspase-8 Inhibitor, Z-IE(OMe)TD(OMe)-FMK) is a specific Caspase-8 inhibitor. Z-IETD-FMK is also an inhibitor of granzyme B. |
- Nat Commun, 2024, 15(1):1282
- J Immunother Cancer, 2024, 12(10)e009032
- Mol Metab, 2024, 87:101988
|
|
S7775 |
Emricasan (IDN-6556)
|
Emricasan (IDN-6556, PF 03491390, PF-03491390) is a potent irreversible pan-caspase inhibitor. Emricasan is an inhibitor of Zika virus infection. |
- Immunity, 2024, S1074-7613(24)00221-8
- Acta Neuropathol, 2024, 147(1):56
- Cell Death Differ, 2024, 31(7):938-953
|
|
S7901 |
Ac-DEVD-CHO
|
Ac-DEVD-CHO (Caspase-3 Inhibitor I, N-Ac-Asp-Glu-Val-Asp-CHO) is a potent aldehyde inhibitor of Group II caspases with Ki values of 0.2 nM and 0.3 nM for for caspase-3 and caspase-7, respectively. Weak inhibition for caspase-2. |
- Environ Pollut, 2024, 345:123467
- Int J Mol Sci, 2024, 25(1)627
- Cell, 2023, 186(14):3033-3048.e20
|
|
S7313 |
Z-LEHD-FMK TFA
|
Z-LEHD-FMK TFA (Caspase-9 Inhibitor) is a cell-permeable, competitive and irreversible inhibitor of enzyme caspase-9, which helps in cell survival. |
- Front Immunol, 2024, 15:1384606
- Ecotoxicol Environ Saf, 2024, 284:116944
- PLoS Pathog, 2024, 20(4):e1012146
|
|
S8102 |
Z-VAD(OH)-FMK (Caspase Inhibitor VI)
|
Z-VAD(OH)-FMK (Caspase Inhibitor VI) is an irreversible pan-caspase inhibitor. |
- Cell, 2024, 187(15):4043-4060.e30
- Nat Commun, 2024, 15(1):9464
- J Ethnopharmacol, 2024, 328:118057
|
|
S8507 |
Z-YVAD-FMK
|
Z-YVAD-FMK is a cell-permeable and irreversible caspase-1 specific inhibitor with anti-inflammatory and anti-tumor activities. |
- Transl Psychiatry, 2024, 14(1):166
- EMBO J, 2023, e113118.
- J Nanobiotechnology, 2023, 21(1):426
|
|
S2417 |
20-Hydroxyecdysone
|
20-Hydroxyecdysone (Ecdysterone, 20E, B-ecdysone, Commisterone, Crustecdysone) is a naturally occurring ecdysteroid hormone which controls the ecdysis (moulting) and metamorphosis of arthropods.20-Hydroxyecdysone (Ecdysterone, 20E) inhibits caspase activity and induces autophagy via the 20E nuclear receptor complex, EcR-USP. |
- bioRxiv, 2024, 10.1101/2024.01.04.574133
- Appl Sci, 2023, 13(2), 860
- Biomed Environ Sci, 2022, 35(6):504-517
|
|
S9042 |
Wedelolactone
|
Wedelolactone, a medicinal plant-derived natural compound, is an inhibitor of IKK that is critical for activation of NF-κB by mediating phosphorylation and degradation of IκBα. Wedelolactone is also an inhibitor of caspase-11. |
- Int J Ophthalmol, 2024, 17(4):616-624
- PeerJ, 2022, 10:e13766
- Exp Eye Res, 2021, 211:108750
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S3275 |
Senkyunolide I
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Senkyunolide I (SEI, SENI) is an orally active compound isolated from Ligusticum chuanxiong with analgesic, anti-migraine, neuroprotective, anti-oxidation and anti-apoptosis activities. Senkyunolide I (SEI, SENI) up-regulates the phosphorylation of Erk1/2 and induces Nrf2 nuclear translocation with enhanced HO-1 and NQO1 expressions. Senkyunolide I (SEI, SENI) promotes the ratio of Bcl-2/Bax and inhibits the expressions of cleaved caspase 3 and caspase 9. |
- World J Emerg Med, 2024, 15(3):206-213
- SSRN , 2024, 10.2139/ssrn.4696834
- Cancer Biol Med, 2022, 19(11)j.issn.2095-3941.2022.0451
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S9817 |
Ac-FLTD-CMK
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Ac-FLTD-CMK is a specific inhibitor for inflammatory caspases. Ac-FLTD-CMK inhibits gasdermin D (GSDMD) cleavage by caspases-1, -4, -5, and -11 in vitro. Ac-FLTD-CMK is effective against caspases-1, caspases-4 and caspases-5 with IC50 of 46.7 nM, 1.49 μM and 329 nM, respectively. |
- Cell Death Discov, 2024, 10(1):416
- Biomolecules, 2022, 12(11)1660
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E3053 |
Mentha Arvensis Leaf Extract
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Mentha Arvensis Leaf Extract is extracted from the leaf of Mentha Arvensis, which might be considered as a promising anticancer agent in breast cancer therapy in combination with synthesised GSNPs because they are less toxic and nonmutagenic and mediate caspase 9-dependent apoptosis. |
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E3835 |
Cordyceps Militaris Extract
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Cordyceps Militaris Extract is extracted from Cordyceps militaris, which induces apoptosis and pyroptosis via caspase-3 and can be used as an anticancer agent. |
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S3267 |
Nicotiflorin (Kaempferol-3-O-rutinoside)
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Nicotiflorin (Kaempferol-3-O-rutinoside), a flavonoid extracted from Carthamus tinctorius, alters the shape and structure of injured neurons, decreases the number of apoptotic cells, down-regulates expression of p-JAK2, p-STAT3, caspase-3, and Bax and decreases Bax immunoredactivity, and increases Bcl-2 protein expression and immunoreactivity. |
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E2354 |
Valepotriate
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Valepotriate, an unstable iridoid isolated from Valeriana jatamansi Jones, has anti-epileptic by significantly increasing the expression of GABAA, glutamic acid decarboxylase 65, and Bcl-2 and reduce the expression of caspase-3. |
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S9075 |
Mulberroside A
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Mulberroside A, isolated from the ethanol extract of Morus alba roots, is widely employed as an active ingredient in cosmetic products due to its anti-tyrosinase and anti-oxidant activities. Mulberroside A decreases the expressions of TNF-α, IL-1β and IL-6 and inhibits the activation of NALP3, caspase-1 and NF-κB and the phosphorylation of ERK, JNK and p38. |
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S5579 |
Chelidonic acid
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Chelidonic acid (Jerva acid, Jervaic acid, γ-Pyrone-2,6-dicarboxylic acid) is a secondary metabolite found in several plants with therapeutic potential in allergic disorders in experimental animals. Chelidonic acid inhibits IL-6 production by blocking NF-κB and caspase-1 in HMC-1 cells. Chelidonic acid is also an inhibitor of glutamate decarboxylase with Ki of 1.2 μM. |
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S5584 |
Citronellol
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Citronellol (Dihydrogeraniol, (±)-β-Citronellol), a constituent of rose and geranium oils, is used in perfumes and insect repellents. Citronellol can cause necrotic apoptosis of NCI-H1299 cells by up-regulating TNF-α, RIP1 / RIP3 activities, and down-regulating caspase-3 / caspase-8 activities. Citronellol also results in a biphasic increase in ROS production at 1 h and at 12 h in NCI-H1299 cells. |
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S6846 |
Gly-Phe β-naphthylamide
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Gly-Phe β-naphthylamide (Gly-Phe beta-naphthylamide) is a substrate of cathepsin C that accumulates within the lysosome. Gly-Phe-β-naphthylamide can inhibit the cathepsin-dependent activation of caspase-8. |
- Anticancer Res, 2024, 44(9):3793-3798
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S1029 |
Lenalidomide
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Lenalidomide is a TNF-α secretion inhibitor with IC50 of 13 nM in PBMCs. Lenalidomide (CC-5013) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide promotes cleaved caspase-3 expression and inhibit VEGF expression and induces apoptosis. |
- Nat Commun, 2024, 15(1):9559
- Nat Commun, 2024, 15(1):7388
- Clin Immunol, 2024, 260:109915
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S2768 |
Dinaciclib
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Dinaciclib is a novel and potent CDK inhibitor for CDK2, CDK5, CDK1 and CDK9 with IC50 of 1 nM, 1 nM, 3 nM and 4 nM in cell-free assays, respectively. It also blocks thymidine (dThd) DNA incorporation. Dinaciclib induces apoptosis through the activation of caspases 8 and 9. Phase 3. |
- Cell Death Dis, 2024, 15(4):285
- Cell Death Dis, 2024, 15(5):345
- Cell Death Dis, 2024, 15(4):285
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S2891 |
GW441756
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GW441756 is a potent, selective inhibitor of TrkA with IC50 of 2 nM, with very little activity to c-Raf1 and CDK2. GW441756 produces a relevant increase of caspase-3 that leads to apoptosis. |
- Cells, 2023, 12(3)373
- Cells, 2023, 12(3):373
- J Cell Mol Med, 2023, 10.1111/jcmm.17906
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S2738 |
PAC-1
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PAC-1 is a potent procaspase-3 activator with EC50 of 0.22 μM and the first small molecule known to directly activate procaspase-3 to caspase-3. |
- Nat Commun, 2023, 14(1):5773
- Nat Commun, 2023, 14(1):5773
- Microb Cell, 2023, 10(8):157-169
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S2927 |
Apoptosis Activator 2
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Apoptosis Activator 2 strongly induces caspase-3 activation, PARP cleavage, and DNA fragmentation which leads to the destruction of cells (Apaf-1 dependent) with IC50 of ~4 μM, inactive to HMEC, PREC, or MCF-10A cells. |
- BMC Mol Cell Biol, 2023, 24(1):14
- BMC Mol Cell Biol, 2023, 24(1):14
- Antioxidants (Basel), 2021, 10(2)184
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S2448 |
Gambogic Acid
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Gambogic Acid (Guttatic Acid, Guttic Acid, Beta-Guttiferrin) activates caspases with EC50 of 0.78-1.64 μM and competitively inhibits Bcl-XL, Bcl-2, Bcl-W, Bcl-B, Bfl-1 and Mcl-1 with IC50 of 1.47, 1.21, 2.02, 0.66, 1.06 and 0.79 μM, respectively. |
- Cells, 2023, 12(18)2247
- Cells, 2023, 10.3390/cells12182247
- Cancers (Basel), 2022, 14(22)5505
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S5967 |
Berberine chloride hydrate
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Berberine (Natural Yellow 18) chloride hydrate is a quaternary ammonium salt from the group of isoquinoline alkaloids. Berberine activates caspase 3 and caspase 8, cleavage of poly ADP-ribose polymerase (PARP) and the release of cytochrome c. Berberine chloride decreases the expression of c-IAP1, Bcl-2 and Bcl-XL. Berberine chloride induces apoptosis with sustained phosphorylation of JNK and p38 MAPK, as well as generation of the ROS. Berberine chloride is a dual topoisomerase I and II inhibitor. Berberine chloride is also a potential autophagy modulator. |
- Front Biosci (Landmark Ed), 2022, 27(8):242
- Front Pharmacol, 2021, 12:632201
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S3865 |
Taurochenodeoxycholic acid
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Taurochenodeoxycholic acid (Taurochenodeoxycholate, TCDCA, Chenodeoxycholyltaurine), a bile acid formed in the liver of most species, is used as a cholagogue and choleretic. |
- Nat Commun, 2021, 12(1):6479
- Microbiome, 2019, 7(1):145
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S7326 |
Tasisulam
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Tasisulam (LY573636) is an antitumor agent and an apoptosis inducer via the intrinsic pathway. Phase 3. |
- Skin Pharmacol Physiol, 2016, 29(6):281-290
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S3238 |
Resibufogenin
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Resibufogenin (Bufogenin, Recibufogenin), a component of huachansu with anticancer effect, triggers necroptosis through upregulating receptor-interacting protein kinase 3 (RIP3) and phosphorylating mixed lineage kinase domain-like protein at Ser358. Resibufogenin exerts cytotoxic effect by inducing reactive oxygen species (ROS) accumulation. Resibufogenin induces apoptosis and caspase-3 and caspase-8 activity. Resibufogenin increases Bax/Bcl-2 expression, and suppresses cyclin D1, cyclin E, PI3K, p-AKT, p-GSK3β and β-catenin protein expression. |
- Research Square, 2024, 10.21203/rs.3.rs-3790060/v1
- Phytomedicine, 2022, 102:154182
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S0563 |
10-Deacetyl-7-xylosyl paclitaxel
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10-Deacetyl-7-xylosyl paclitaxel (10-Deacetyl-7-xylosyltaxol, 7-xylosyl-10-deacetylpaclitaxel), a derivative of paclitaxel and naturally occurring xyloside isolated from Taxus chinensis, causes significant mitotic arrest in PC-3 cells followed by up-regulating expression of pro-apoptotic Bax and Bad protein, as well as down-regulating expression of anti-apoptotic Bcl-2 and Bcl-XL , which leads to a disturbance of the mitochondrial membrane permeability and to the activation of caspase-9. |
- Cell Death Dis, 2022, 13-9:799
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S9634 |
Phenoxodiol (Haginin E)
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Phenoxodiol (Haginin E, Idronoxil, Dehydroequol, NV 06, PXD) is an isoflavone analog with antineoplastic activity that activates the caspase system, inhibits XIAP (X-linked inhibitor of apoptosis), and disrupts FLICE inhibitory protein (FLIP) expression, resulting in tumor cell apoptosis. Phenoxodiol also inhibits DNA topoisomerase II. |
- Anticancer Res, 2018, 38(10):5709-5716
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E3037 |
Solanum lyratum Extract
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Solanum lyratum Extract (300 μg/ml) increases Bax levels and decreases Bcl-2 levels, which cause the loss of mitochondrial membrane potential (Δæm) followed by cytochrome C release and caspase-9 and -3 activation, finally leading to apoptosis. Solanum lyratum Extract (300 μg/ml) also promotes p53 and p27, but decreases the levels of cyclin B1 thus causing S-phase arrest. |
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S6899 |
Licochalcone D
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Licochalcone D (Lico D, LCD, LD), a flavonoid isolated from a Chinese medicinal plant Glycyrrhiza inflata, has antioxidant, anti-inflammatory and anti-cancer properties. Licochalcone D inhibit phosphorylation of NF-κB p65 in LPS signaling pathway. Licochalcone D inhibits JAK2, EGFR and Met (c-Met) activities and induces ROS-dependent apoptosis. Licochalcone D also induces caspases activation and poly (ADP-ribose) polymerase (PARP) cleavage. |
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S0913 |
4',5,7-Trimethoxyflavone
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4',5,7-Trimethoxyflavone (5,7,4'-Trimethoxyflavone, TMF) is a flavonoid isolated from Kaempferia parviflora (KP) that induces apoptosis. 4',5,7-Trimethoxyflavone increases sub-G1 phase, DNA fragmentation, annexin-V/PI staining and Bax/Bcl-xL ratio, activates caspase-3 and degrades poly (ADP-ribose) polymerase (PARP) protein. |
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S6501 |
NVP 231
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NVP 231 is a novel CerK inhibitor that inhibits the catalytic activity of recombinant CerK in vitro with an IC50 of 12 nM. NVP 231 induces cell apoptosis by increasing DNA fragmentation and caspase-3 and caspase-9 cleavage. |
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S9276 |
Alisol B
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Alisol B, a triterpene from Alismatis rhizoma, induces Bax up-regulation and nuclear translocation, the activation of initiator caspase-8 and caspase-9, and executor caspase-3, suggesting the involvement of both extrinsic and intrinsic apoptosis pathways. |
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S2271 |
Berberine chloride
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Berberine chloride is a quaternary ammonium salt from the group of isoquinoline alkaloids. Berberine activates caspase 3 and caspase 8, cleavage of poly ADP-ribose polymerase (PARP) and the release of cytochrome c. Berberine chloride decreases the expression of c-IAP1, Bcl-2 and Bcl-XL. Berberine chloride induces apoptosis with sustained phosphorylation of JNK and p38 MAPK, as well as generation of the ROS. Berberine chloride is a dual topoisomerase I and II inhibitor. Berberine chloride is also a potential autophagy modulator. |
- Adv Healthc Mater, 2023, e2300591.
- Transl Oncol, 2023, 35:101712
- J Biomol Struct Dyn, 2022, 1-11
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S0354 |
Alsterpaullone
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Alsterpaullone (Alp, 9-Nitropaullone, NSC 705701) is a potent inhibitor of CDK with IC50 of 35 nM, 15 nM, 200 nM and 40 nM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E and CDK5/p35, respectively. Alsterpaullone also acts as a potent inhibitor of glycogen synthase kinase-3 (GSK-3) with IC50 of both 4 nM for GSK-3α and GSK-3β. Alsterpaullone induces apoptosis by activation of caspase-9. Alsterpaullone has antitumor activity and possesses potential for the treatment of neurodegenerative and proliferative disorders. |
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S4513 |
RGD peptide (GRGDNP)
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RGD peptide (GRGDNP) is an inhibitor of binding of integrins to the extracellular matrixs. RGD peptide (GRGDNP) induces apoptosis presumably through direct activation of caspase-3. |
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S9097 |
Alisol B Acetate
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Alisol B acetate, a triterpene from Alismatis rhizoma, induces Bax up-regulation and nuclear translocation, the activation of initiator caspase-8 and caspase-9, and executor caspase-3, suggesting the involvement of both extrinsic and intrinsic apoptosis pathways. |
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S5550 |
Ethyl gallate
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Ethyl gallat (Phyllemblin, gallic acid ethyl ester), which could be found naturally in a variety of plant sources, is a food additive with antimicrobial activity. Ethyl gallat activates the death receptor-dependent pathway of apoptosis by enhancing the expression of caspases-8, -9, and -3 and the Bcl-2 interacting domain (Bid). |
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S6990 |
Phytohemagglutinin (PHA)
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Phytohemagglutinin (PHA) is expressed in Pichia pastoris using native signal peptides, or the Saccharomyces alpha-factor preprosequence, to direct proteins into the secretory pathway. Phytohemagglutinin induces apoptosis in human HEp-2 carcinoma cells via increasing proapoptotic protein Bax and activating caspases-3. |
- Molecules, 2023, 28(6)2426
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S4353 |
Terfenadine
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Terfenadine is an antihistamine, generally completely metabolizes to the active form fexofenadine in the liver by the enzyme cytochrome P450 CYP3A4 isoform. Terfenadine ((±)-Terfenadine) is a potent open-channel blocker of hERG with an IC50 of 204 nM. Terfenadine, an H1 histamine receptor antagonist, acts as a potent apoptosis inducer in melanoma cells through modulation of Ca2+ homeostasis. Terfenadine induces ROS-dependent apoptosis, simultaneously activates Caspase-4, -2, -9. |
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